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体内磺酰氟生物转化的分析和鉴定。

Profiling and Identification of Biocatalyzed Transformation of Sulfoxaflor In Vivo.

机构信息

State Key Laboratory of Food Science and Technology, Jiangnan University, Wuxi, Jiangsu, 214122, P. R. China.

International Joint Research Laboratory for Bi ointerface and Biodetection and School of Food Science and Technology, Jiangnan University, Wuxi, Jiangsu, 214122, P. R. China.

出版信息

Angew Chem Int Ed Engl. 2020 Sep 7;59(37):16218-16224. doi: 10.1002/anie.202007079. Epub 2020 Jun 29.

Abstract

In the present study, we investigated the biotransformation of the neonicotinoid pesticide sulfoxaflor and the metabolic responses in Sprague-Dawley rats. Sulfoxaflor transformation was catalyzed by cytochrome P450 while five phase I and four phase II metabolites were identified for the first time in vivo. The experimental results demonstrated that sulfoxaflor brought about the metabolic profiling disturbances in liver and bile. Exposure to sulfoxaflor caused dysregulation of bile acid synthesis and reabsorption by the expression of farnesoid X receptor (FXR). Our data provided insights into biotransformation of chemicals while enabling the implementation of a new toolbox for the design of sulfoximine compounds.

摘要

在本研究中,我们研究了新烟碱类杀虫剂噻虫啉的生物转化以及 Sprague-Dawley 大鼠的代谢反应。噻虫啉的转化由细胞色素 P450 催化,同时首次在体内鉴定出五种 I 相和四种 II 相代谢物。实验结果表明,噻虫啉导致肝脏和胆汁的代谢谱紊乱。暴露于噻虫啉会通过法尼醇 X 受体(FXR)的表达引起胆汁酸合成和重吸收的失调。我们的数据为化学物质的生物转化提供了深入的了解,同时为噻虫啉肟类化合物的设计提供了一个新的工具包。

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